生理学报
生理學報
생이학보
ACTA PHYSIOLOGICA SINICA
2000年
3期
247-251
,共5页
多巴胺受体%cAMP%血管床%fenoldopam%propy1-butyl-dopamine (PBDA)%SCH23390%domperidone
多巴胺受體%cAMP%血管床%fenoldopam%propy1-butyl-dopamine (PBDA)%SCH23390%domperidone
다파알수체%cAMP%혈관상%fenoldopam%propy1-butyl-dopamine (PBDA)%SCH23390%domperidone
dopamine receptors%cyclic AMP%vascular system%fenoldopam%propy1-butyl-dopamine (PBDA)%SCH23390%domperidone
实验观察了选择性多巴胺(DA)DA1受体激动剂fenoldopam与DA2受体激动剂propy1-butyl-dopamine (PBDA)对兔肾动脉, 肺、肠系膜动脉和股动脉环磷酸腺苷(cAMP)产生系统的影响.结果表明: (1)除股动脉外, fenoldopam均可浓度依赖性地增加肺动脉、肾动脉和肠系膜动脉cAMP的生成量.选择性DA1受体阻断剂SCH23390可以显著阻断fenoldopam的效应, 而DA2受体阻断剂domperidone则对fenoldopam的这一效应不产生任何影响.(2) PBDA可浓度依赖性地降低股动脉的cAMP生成量, 又可浓度依赖性地激活肠系膜动脉、肺动脉和肾动脉的腺苷酸环化酶(AC)活性, 增加cAMP的生成量.(3) domperidone 可明显减小PBDA对股动脉AC活性的抑制效应, 并可使PBDA对肠系膜动脉AC活性效应增强, 但不改变PBDA对肾动脉和肺动脉的AC活性效应.(4) SCH23390不影响PBDA对股动脉AC活性的抑制效应, 可显著降低PBDA对肾动脉、肺动脉和肠系膜动脉激活AC活性的效应, cAMP的含量显著减小.以上结果提示, 在肺动脉、肾动脉和肠系膜动脉上存在DA1受体介导的cAMP产生系统, 而在股动脉仅有DA2受体介导的cAMP产生系统.在肠系膜动脉既存在DA2受体介导的cAMP产生系统, 又存在DA1受体介导的cAMP产生系统.PBDA既有通过刺激DA2受体抑制AC活性的作用, 又有刺激DA1受体而激活AC活性、增加cAMP的效应.
實驗觀察瞭選擇性多巴胺(DA)DA1受體激動劑fenoldopam與DA2受體激動劑propy1-butyl-dopamine (PBDA)對兔腎動脈, 肺、腸繫膜動脈和股動脈環燐痠腺苷(cAMP)產生繫統的影響.結果錶明: (1)除股動脈外, fenoldopam均可濃度依賴性地增加肺動脈、腎動脈和腸繫膜動脈cAMP的生成量.選擇性DA1受體阻斷劑SCH23390可以顯著阻斷fenoldopam的效應, 而DA2受體阻斷劑domperidone則對fenoldopam的這一效應不產生任何影響.(2) PBDA可濃度依賴性地降低股動脈的cAMP生成量, 又可濃度依賴性地激活腸繫膜動脈、肺動脈和腎動脈的腺苷痠環化酶(AC)活性, 增加cAMP的生成量.(3) domperidone 可明顯減小PBDA對股動脈AC活性的抑製效應, 併可使PBDA對腸繫膜動脈AC活性效應增彊, 但不改變PBDA對腎動脈和肺動脈的AC活性效應.(4) SCH23390不影響PBDA對股動脈AC活性的抑製效應, 可顯著降低PBDA對腎動脈、肺動脈和腸繫膜動脈激活AC活性的效應, cAMP的含量顯著減小.以上結果提示, 在肺動脈、腎動脈和腸繫膜動脈上存在DA1受體介導的cAMP產生繫統, 而在股動脈僅有DA2受體介導的cAMP產生繫統.在腸繫膜動脈既存在DA2受體介導的cAMP產生繫統, 又存在DA1受體介導的cAMP產生繫統.PBDA既有通過刺激DA2受體抑製AC活性的作用, 又有刺激DA1受體而激活AC活性、增加cAMP的效應.
실험관찰료선택성다파알(DA)DA1수체격동제fenoldopam여DA2수체격동제propy1-butyl-dopamine (PBDA)대토신동맥, 폐、장계막동맥화고동맥배린산선감(cAMP)산생계통적영향.결과표명: (1)제고동맥외, fenoldopam균가농도의뢰성지증가폐동맥、신동맥화장계막동맥cAMP적생성량.선택성DA1수체조단제SCH23390가이현저조단fenoldopam적효응, 이DA2수체조단제domperidone칙대fenoldopam적저일효응불산생임하영향.(2) PBDA가농도의뢰성지강저고동맥적cAMP생성량, 우가농도의뢰성지격활장계막동맥、폐동맥화신동맥적선감산배화매(AC)활성, 증가cAMP적생성량.(3) domperidone 가명현감소PBDA대고동맥AC활성적억제효응, 병가사PBDA대장계막동맥AC활성효응증강, 단불개변PBDA대신동맥화폐동맥적AC활성효응.(4) SCH23390불영향PBDA대고동맥AC활성적억제효응, 가현저강저PBDA대신동맥、폐동맥화장계막동맥격활AC활성적효응, cAMP적함량현저감소.이상결과제시, 재폐동맥、신동맥화장계막동맥상존재DA1수체개도적cAMP산생계통, 이재고동맥부유DA2수체개도적cAMP산생계통.재장계막동맥기존재DA2수체개도적cAMP산생계통, 우존재DA1수체개도적cAMP산생계통.PBDA기유통과자격DA2수체억제AC활성적작용, 우유자격DA1수체이격활AC활성、증가cAMP적효응.
Effects of selective dopamine-1 (DA1) receptor agonist fenoldopam and dopamine-2 (DA2) receptor agonist propy1-butyl-dopamine (PBDA) on the cAMP generation system in renal, pulmonary, mesenteric and femoral arteries of rabbits were studied. The results are as follows. (1) Fenoldopam increased the cAMP production in a dose-dependent manner in pulmonary, renal and mesenteric arteries. This effect of fenoldopam was markedly blocked by specific DA1 receptor antagonist SCH23390, but not at all by specific DA2 receptor antagonist domperidone. (2) PBDA induced a dose-dependent decrease in cAMP content in femoral artery. However, the antagonist also moderately increased a dose-dependent cAMP production in mesenteric, pulmonary, and renal arteries. (3) Domperidone significantly decreased the inhibitory effect of PBDA on cAMP production in femoral artery, while it stimulated cAMP production in mesenteric artery but was of no effect on that in renal and pulmonary arteries. (4) SCH23390 had no effect on the inhibitory action of PBDA in decreasing cAMP content in femoral artery, while it markedly decreased the stimulatory action of PBDA on cAMP production in renal, pulmonary and mesenteric arteries. These findings suggest the presence of DA1 receptors mediating the cAMP generation system in renal, pulmonary and mesenteric arteries, but only DA2 receptors in femoral artery, and both DA1and DA2 receptors in mesenteric artery. PBDA inhibits the AC activity via stimulation of DA2 receptors and increases the AC activity via stimulation of DA1 receptors.
